FLT3

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S2194 R406 <1 mg/mL 100 mg/mL 0 mg/mL
S1526 Quizartinib (AC220) <1 mg/mL 33 mg/mL <1 mg/mL
S1018 Dovitinib (TKI-258, CHIR-258) <1 mg/mL 30 mg/mL <1 mg/mL
S1244 Amuvatinib (MP-470) <1 mg/mL 32 mg/mL <1 mg/mL
S1043 Tandutinib (MLN518) <1 mg/mL 5 mg/mL 6 mg/mL
S7754 Gilteritinib (ASP2215) <1 mg/mL 100 mg/mL 85 mg/mL
S8442 TAK-659 4 mg/mL <1 mg/mL <1 mg/mL
S2692 TG101209 <1 mg/mL 102 mg/mL <1 mg/mL
S2158 KW-2449 <1 mg/mL 67 mg/mL 67 mg/mL
S1181 ENMD-2076 1 mg/mL 105 mg/mL <1 mg/mL
S2769 Dovitinib (TKI-258) Dilactic Acid 70 mg/mL 90 mg/mL <1 mg/mL
S8057 Pacritinib (SB1518) <1 mg/mL 11 mg/mL <1 mg/mL
S8023 TCS 359 <1 mg/mL 15 mg/mL <1 mg/mL
S2018 ENMD-2076 L-(+)-Tartaric acid <1 mg/mL 100 mg/mL <1 mg/mL
S7765 Dovitinib (TKI258) Lactate 66 mg/mL 100 mg/mL 1 mg/mL
S7576 UNC2025 100 mg/mL 25 mg/mL 8 mg/mL
S7545 G-749 <1 mg/mL 24 mg/mL <1 mg/mL
S7003 AZD2932 <1 mg/mL 89 mg/mL 5 mg/mL
S7119 Go6976 <1 mg/mL 18 mg/mL <1 mg/mL
S7533 AMG 925 <1 mg/mL 0.01 mg/mL <1 mg/mL
Catalog No. Information Product Use Citations Product Validations
S2194

R406

R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

S1526

Quizartinib (AC220)

Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 3.

S1018

Dovitinib (TKI-258, CHIR-258)

Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.

S1244

Amuvatinib (MP-470)

Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Phase 2.

S1043

Tandutinib (MLN518)

Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. Phase 2.

S7754New

Gilteritinib (ASP2215)

Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).

S8442New

TAK-659

TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.

S2692

TG101209

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.

S2158

KW-2449

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.

S1181

ENMD-2076

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

S2769

Dovitinib (TKI-258) Dilactic Acid

Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

S8057

Pacritinib (SB1518)

Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

S8023

TCS 359

TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.

S2018

ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

S7765

Dovitinib (TKI258) Lactate

Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

S7576

UNC2025

UNC2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.

S7545

G-749

G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.

S7003

AZD2932

AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.

S7119

Go6976

Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

S7533

AMG 925

AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.

Tags: Flt3 mutation | Flt3 mutations | Flt3 leukemia | Flt3 acute myeloid leukemia | Flt3 receptor | Flt3 signaling | Flt3 cancer | Flt3 inhibitors clinical trials | Flt3 activation | Flt inhibitor review